M62812

M62812 is a toll-like receptor 4 (TLR4) signaling inhibitor. M62812 inhibits endothelial and leukocyte activation and prevents lethal septic shock in mice. M62812 can reduces LPS-induced coagulation and inflammatory responses. M62812 can be used for the research of sepsis^[1]. In Vitro:M62812 (10 μg/mL; 6 h) completely inhibits LPS-induced NF-κB activation in NF-κB luciferase-expressing cells with an IC₅₀ of 2.4 μg/mL^[1].
M62812 (3 μg/mL; 6 h) completely inhibits LPS-induced TNF-α production in peripheral blood mononuclear cells with an IC₅₀ of 0.7 μg/mL^[1].
M62812 (3 μg/mL; 6 h) completely inhibits the production of IL-6 and E-selection in human endothelial cells with IC₅₀s of 0.43 μg/mL and 1.4 μg/mL^[1].
In Vivo:M62812 (i.v.; 10-20 mg/kg; single dose) is protective and reduces inflammatory and coagulation parameters in a D-galactosamine-sensitized endotoxin shock mouse model^[1].
M62812 (i.v.; 20 mg/kg; once a day for three days) prevents mice from lethality in a murine cecal ligation and puncture model^[1].